Abstract

Peptidomimetics with a substituted imidazo[1,2-a]pyridine fragment were synthesized by a tandem of Groebke–Blackburn–Bienaymé and Ugi reactions. The target products contain substituted imidazo[1,2-a]pyridine and peptidomimetic moieties as pharmacophores with four diversity points introduced from readily available starting materials, including scaffold diversity. A small focused compound library of 20 Ugi products was prepared and screened for antibacterial activity.

Beilstein J. Org. Chem. 2023, 19, 727–735. doi:10.3762/bjoc.19.53

中文翻译：

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通过 Groebke–Blackburn–Bienaymé 和 Ugi 反应串联合成含咪唑并 [1,2-a] 吡啶的拟肽

摘要

通过 Groebke-Blackburn-Bienaymé 和 Ugi 反应串联合成具有取代的咪唑并 [1,2- a ] 吡啶片段的拟肽。目标产品包含取代的咪唑并 [1,2- a ] 吡啶和拟肽部分作为药效团，具有从现成的起始材料引入的四个多样性点，包括支架多样性。制备了一个包含 20 种 Ugi 产品的小型重点化合物库，并筛选了抗菌活性。

Beilstein J. Org。化学。 2023, 19, 727–735。doi:10.3762/bjoc.19.53